SB-699551-A (3-cyclopentyl-N-[2-(dimethylamino)ethyl]-N-[(4'-{[(2-phenylethyl)amino]methyl}-4-biphenylyl)methyl]propanamide dihydrochloride), a novel 5-ht5A receptor-selective antagonist, enhances 5-HT neuronal function: Evidence for an autoreceptor role

abstract：:In rats with partial, unilateral lesions of the dopaminergic nigrostriatal pathway, synthesis of dopamine (DA) per surviving neurone was assessed by measuring the ratio of DOPA accumulated after inhibition of aromatic amino acid decarboxylase to dopamine (DOPA/DA ratio). Release of DA per surviving neurone was assesse...

journal_title：Neuropharmacology

authors： Hefti F,Enz A,Melamed E

更新日期：1985-01-01 00:00:00

abstract：:Although there is much evidence for a role of GABAB receptors in the pathophysiology of anxiety, the underlying neuronal mechanisms are largely unclear. The GABAB receptor allosteric positive modulator, GS39783, exerts anxiolytic effects without interfering with GABAB-mediated modulation of body temperature, cognitive...

journal_title：Neuropharmacology

authors： Pizzo R,O'Leary OF,Cryan JF

更新日期：2018-07-01 00:00:00

abstract：:Alterations in motor functions are well-characterized features observed in humans and experimental animals with thyroid hormone dysfunctions during development. We have previously suggested the implication of the endocannabinoid system in the hyperlocomotor phenotype observed in developmentally induced hypothyroidism ...

journal_title：Neuropharmacology

authors： Giné E,Echeverry-Alzate V,Lopez-Moreno JA,Rodriguez de Fonseca F,Perez-Castillo A,Santos A

更新日期：2017-04-01 00:00:00

abstract：:Chronic activity perturbations in neurons induce homeostatic plasticity through modulation of synaptic strength or other intrinsic properties to maintain the correct physiological range of excitability. Although similar plasticity can also occur at the population level, what molecular mechanisms are involved remain un...

journal_title：Neuropharmacology

authors： Jewett KA,Lee KY,Eagleman DE,Soriano S,Tsai NP

更新日期：2018-08-01 00:00:00

abstract：:The mechanisms underlying 3,4-methylenedioxymethamphetamine (MDMA)-induced serotonergic (5-HT) toxicity remain unclear. It has been suggested that MDMA depletes 5-HT by increasing brain tyrosine levels, which via non-enzymatic hydroxylation leads to DA-derived free radical formation. Because this hypothesis assumes th...

journal_title：Neuropharmacology

authors： Goñi-Allo B,Puerta E,Mathúna BO,Hervias I,Lasheras B,de la Torre R,Aguirre N

更新日期：2008-04-01 00:00:00

abstract：:Animal models of inflammatory pain are characterized by the release of inflammatory mediators such as cytokines and neurotrophic factors, and enhanced analgesic sensitivity to opioids. In this study, we examine the mechanisms underlying this effect, in particular the roles of cholecystokinin (CCK) and nerve growth fac...

journal_title：Neuropharmacology

authors： Xanthos DN,Kumar N,Theodorsson E,Coderre TJ

更新日期：2009-03-01 00:00:00

abstract：:The GABAA receptor/chloride ionophore (GABAR) is allosterically modulated by several classes of anticonvulsant agents, including benzodiazepines and barbiturates, and some alkyl-substituted butyrolactones. To test the hypothesis that the anticonvulsant butyrolactones act at a distinct positive-modulatory site on the G...

journal_title：Neuropharmacology

authors： Mathews GC,Bolos-Sy AM,Covey DF,Rothman SM,Ferrendelli JA

更新日期：1996-02-01 00:00:00

abstract：:N-methyl-d-aspartate (NMDA) receptors composed of glycine-binding GluN1 and GluN3 subunits function as excitatory glycine receptors that respond to agonist application only with a very low efficacy. Binding of glycine to the high-affinity GluN3 subunits triggers channel opening, whereas glycine binding to the low-affi...

journal_title：Neuropharmacology

authors： Mesic I,Madry C,Geider K,Bernhard M,Betz H,Laube B

更新日期：2016-06-01 00:00:00

abstract：:Benzodiazepines (BZDs) are widely used in the treatment of a variety of neurological and psychiatric conditions including anxiety, insomnia and epilepsy. BZDs are thought to act predominantly by affecting the gating of GABAA receptor channels, resulting in enhanced GABA-mediated currents in neurons. However, mutations...

journal_title：Neuropharmacology

authors： Lévi S,Le Roux N,Eugène E,Poncer JC

更新日期：2015-01-01 00:00:00

abstract：:1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), or 0.9% saline, was administered to a group of common marmosets initially treated with the toxin 12-18 months previously. Initial treatment had consisted of a cumulative dose of 6-22 mg/kg (i.p.) which caused marked parkinsonism. Subsequently, the animals gradually ...

journal_title：Neuropharmacology

authors： Ueki A,Chong PN,Albanese A,Rose S,Chivers JK,Jenner P,Marsden CD

更新日期：1989-10-01 00:00:00

abstract：:This study investigated the structure-activity relationships and kinetic properties of a library of kynurenate analogues as inhibitors of 3H-L-glutamate transport into rat forebrain synaptic vesicles. The lack of inhibitory activity observed with the majority of the monocyclic pyridine derivatives suggested that the s...

journal_title：Neuropharmacology

authors： Bartlett RD,Esslinger CS,Thompson CM,Bridges RJ

更新日期：1998-07-01 00:00:00

abstract：:The effects of thyrotropin-releasing hormone (TRH) and an analog of this hormone, MK-771, were determined on body shaking behavior and on biochemical estimates of the activity of dopamine (DA) neurons in the rat. Both compounds elicited dose-related episodes of "wet-dog shakes". A dose of TRH (20 mg/kg, i.p.) which ca...

journal_title：Neuropharmacology

authors： Yamada K,Demarest KT,Moore KE

更新日期：1984-07-01 00:00:00

abstract：:Following injection of 5 micrograms of the competitive NMDA receptor antagonist AP-5 into the nucleus accumbens of monoamine-depleted mice a pronounced locomotor stimulation was produced. Additional treatment with an intraperitoneal (i.p.) injection of the alpha-adrenoceptor agonist clonidine markedly increased the lo...

journal_title：Neuropharmacology

authors： Svensson A,Carlsson ML

更新日期：1992-05-01 00:00:00

abstract：:Hippocampal damage produces spatial memory impairment and hyperactivity in animals, while reductions in hippocampal size have been associated with memory deficits in humans. There are no known treatments for the behavioral changes specifically related to reduced hippocampal size. The purpose of this study was to deter...

journal_title：Neuropharmacology

authors： Bardgett ME,Baum KT,O'Connell SM,Lee NM,Hon JC

更新日期：2006-12-01 00:00:00

abstract：:Chronic nicotine administration in animals, and smoking in humans, causes up-regulation of α4β2* neuronal nicotinic receptors (nAChRs), which has been hypothesized to contribute to the addictive actions of nicotine. We used a rat model to test whether such up-regulatory effects differ in adolescents versus adults, and...

journal_title：Neuropharmacology

authors： Hoegberg BG,Lomazzo E,Lee NH,Perry DC

更新日期：2015-12-01 00:00:00

abstract：:The effect of drugs which down-regulate the function of GABA at the level of the GABA/benzodiazepine receptor complex was studied on the conflict test in the rat. The GABA receptor antagonist, bicuculline, and the blockers of the GABA-receptor-coupled chloride channel, picrotoxin and pentylenetetrazol, produced a dose...

journal_title：Neuropharmacology

authors： Corda MG,Biggio G

更新日期：1986-05-01 00:00:00

abstract：:Central administration of corticotropin-like peptides generally blocks the analgesic action of opiate ligands, yet it is unclear whether this is due to an independent hyperalgesic action of corticotropin or to some other mechanism. Single cells in the ventromedial medulla of the anaesthetized rat were characterized as...

journal_title：Neuropharmacology

authors： Smock T

更新日期：1987-12-01 00:00:00

abstract：:A unique type of limbic seizures, maximal dentate activation, was used to examine the effects of cholinergic and adrenergic agents on the processes involved in epileptogenesis. The time to onset of maximal dentate activation was used to monitor the initiation of seizures while the duration of maximal dentate activatio...

journal_title：Neuropharmacology

authors： Stringer JL,Lothman EW

更新日期：1991-01-01 00:00:00

abstract：:Several psychiatric disorders involving the prefrontal cortex (PFC) are associated with a dysfunction of 5-HT(1A) receptors (5-HT(1A)R). These receptors, located on interneurons and pyramidal neurons, may influence neuronal excitability through a regulation of the balance between excitation (E) and inhibition (I). Pat...

journal_title：Neuropharmacology

authors： Meunier CN,Amar M,Lanfumey L,Hamon M,Fossier P

更新日期：2013-08-01 00:00:00

abstract：:Previous investigations have shown that mGlu receptors would be involved in the amphetamine-induced motor response. However, data are somewhat controversial across studies where methodological protocols vary. The aim of the present study was to determine the involvement of mGlu receptors in the NAcc in the locomotor-a...

journal_title：Neuropharmacology

authors： David HN,Abraini JH

更新日期：2003-05-01 00:00:00

abstract：:Brain preconditioning is a protective mechanism, which can be activated by sub-lethal stimulation of the NMDA receptors (NMDAR) and be used to achieve neuroprotection against stroke and neurodegenerative diseases models. Inhibitors of glycine transporters type 1 modulate glutamatergic neurotransmission through NMDAR, ...

journal_title：Neuropharmacology

authors： Pinto MC,Lima IV,da Costa FL,Rosa DV,Mendes-Goulart VA,Resende RR,Romano-Silva MA,de Oliveira AC,Gomez MV,Gomez RS

更新日期：2015-02-01 00:00:00

abstract：:Nitronyl nitroxides (NN) effectively decompose free radicals (. As brain endothelium, forming the blood-brain barrier (BBB), is both the main source and the target of reactive species during cerebral oxidative stress, we studied the effect of NN on brain endothelial cells injured by the mediator of oxidative stress H(...

journal_title：Neuropharmacology

authors： Blasig IE,Mertsch K,Haseloff RF

更新日期：2002-11-01 00:00:00

abstract：:Neurosteroids are synthesized in the brain and have been demonstrated to modulate various cerebral functions. Allopregnanolone (3alpha-hydroxy-5alpha-pregnan-20-one), a naturally occurring neurosteroid, and ganaxolone (3alpha-hydroxy-3beta-methyl-5alpha-pregnan-20-one), a synthetic derivative, are two neurosteroids ac...

journal_title：Neuropharmacology

authors： Citraro R,Russo E,Di Paola ED,Ibbadu GF,Gratteri S,Marra R,De Sarro G

更新日期：2006-06-01 00:00:00

abstract：:A pharmacological study using monkeys, in which parkinsonism was induced by 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), was undertaken to elucidate the mechanism underlying urinary bladder dysfunctions in Parkinson's disease. Under ketamine anesthesia, cystometrograms showed that, in MPTP-treated monkeys, a c...

journal_title：Neuropharmacology

authors： Yoshimura N,Mizuta E,Kuno S,Sasa M,Yoshida O

更新日期：1993-04-01 00:00:00

abstract：:The interest in the role of metabotropic glutamate receptor 4 (mGlu4) in CNS related disorders has increased the need for methods to investigate the binding of allosteric drug candidates. Our aim is to present the first fully characterized in vitro binding assay of mGlu4 positive allosteric modulators (PAMs). Results ...

journal_title：Neuropharmacology

authors： Poutiainen P,Kil KE,Zhang Z,Kuruppu D,Tannous B,Brownell AL

更新日期：2015-10-01 00:00:00

abstract：:While evidence indicates that sigma-1 receptors (Sig-1Rs) play an important role in the induction of peripheral neuropathic pain, there is limited understanding of the role that the neurosteroidogenic enzymes, which produce Sig-1R endogenous ligands, play during the development of neuropathic pain. We examined whether...

journal_title：Neuropharmacology

authors： Choi SR,Roh DH,Yoon SY,Choi HS,Kang SY,Han HJ,Beitz AJ,Lee JH

更新日期：2019-05-01 00:00:00

abstract：:The rat hemisected spinal cord preparation was used to assess the role of different adrenoceptor subtypes on the modulation of nociceptive reflexes. These were elicited by trains of high intensity electrical stimuli delivered to a lumbar dorsal root. Responses were recorded from the corresponding ventral root in AC- a...

journal_title：Neuropharmacology

authors： Hedo G,Lopez-Garcia JA

更新日期：2001-12-01 00:00:00

abstract：:Rats were given daily injections of increasing doses of morphine sulfate (40-100 mg/kg, s.c.), for 4 days. Twenty hours after the last injection of morphine, the animals received bilateral injections of naloxone (1-10 micrograms) into the substantia nigra, ventral tegmental area or sites 2 mm rostral, caudal or dorsal...

journal_title：Neuropharmacology

authors： Baumeister AA,Anticich TG,Hebert G,Hawkins MF,Nagy M

更新日期：1989-11-01 00:00:00

abstract：:There has been increasing interest in the rostromedial tegmental nucleus (RMTg), given its potential regulatory role in many aversion-related behaviors. The RMTg contains mostly GABAergic neurons, sends a dense inhibitory projection to dopamine neurons in the midbrain, and is rich with μ-opioid receptors (MOR). Like m...

journal_title：Neuropharmacology

authors： Fu R,Chen X,Zuo W,Li J,Kang S,Zhou LH,Siegel A,Bekker A,Ye JH

更新日期：2016-08-01 00:00:00

abstract：:The role in ligand recognition and receptor activation of two adjacent charged residues (lysine 195 and aspartate 196) in the first extracellular loop of the human VPAC(1) receptor was investigated in stably transfected CHO cells expressing the wild type or point mutated receptors.Replacement of lysine 195 by glutamin...

journal_title：Neuropharmacology

authors： Langer I,Vertongen P,Perret J,Waelbroeck M,Robberecht P

更新日期：2003-01-01 00:00:00